Chemical Papers

, Volume 73, Issue 1, pp 39–46 | Cite as

Improved protocol for synthesis of N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy) quinazolin-4-amine (gefitinib)

  • Pawan KumarEmail author
  • Muhammad Taufiq F. Mazlee
  • Muhammad K. Abdul Wahab
  • Chandra Kant Belwal
  • Ramesh Kumar
  • Shahnawaz Sajid
Original Paper


An improved three-step process for the synthesis of gefitinib from readily available starting material is discussed in this protocol. The protocol is based on the synthesis, isolation, characterization of novel intermediates and their application in the alkylation step for the synthesis of gefitinib. Excellent results were achieved over the conventional synthetic methodologies. Isolation of these intermediates were effective in replacing high boiling solvent with low boiling solvent(s) but also in eliminating base from the reaction. These conditions led to effective elimination of all the prior art reported impurities. This high-yielding process is cost-effective with isolable and stable intermediates. These intermediates were characterized using NMR, mass spectroscopy, DSC and XRPD analyses.


Gefitinib Iressa Alkali metal salts O-Alkylation Novel intermediate Improved protocol 

Supplementary material

11696_2018_564_MOESM1_ESM.pdf (605 kb)
Supplementary material 1 (PDF 605 kb)


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Copyright information

© Institute of Chemistry, Slovak Academy of Sciences 2018

Authors and Affiliations

  1. 1.Oncogen Pharma Sdn BhdShah AlamMalaysia

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